JP5857136B2 - ｍＧｌｕＲ２−陰性アロステリック調節因子としてのキノリンカルボキサミドおよびキノリンカルボニトリル誘導体、組成物、およびその使用 - Google Patents

ｍＧｌｕＲ２−陰性アロステリック調節因子としてのキノリンカルボキサミドおよびキノリンカルボニトリル誘導体、組成物、およびその使用 Download PDF

Info

Publication number
JP5857136B2
JP5857136B2 JP2014539998A JP2014539998A JP5857136B2 JP 5857136 B2 JP5857136 B2 JP 5857136B2 JP 2014539998 A JP2014539998 A JP 2014539998A JP 2014539998 A JP2014539998 A JP 2014539998A JP 5857136 B2 JP5857136 B2 JP 5857136B2
Authority
JP
Japan
Prior art keywords
alkyl
mmol
methyl
quinoline
group
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2014539998A
Other languages
English (en)
Japanese (ja)
Other versions
JP2015501783A5 (enExample
JP2015501783A (ja
Inventor
バンガード，クリストフアー・ジエイムズ
コンベルソ，アントネラ
デ・レオン，パブロ
ハンニイ，バーバラ
ハーテイング，テイモシー・ジヨン
マニコウスキー，ジエス・ジヨセフ
マンレイ，ペーター，ジエイ
マイスナー，ロバート
ムオン，ジヤオヤ−ン
ペーキンズ，ジエイムズ，ジエイ
ルツド，マイケル，テイー
シユウ，ヨウホーン
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp & Dohme LLC
Original Assignee
Merck Sharp & Dohme LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Sharp & Dohme LLC filed Critical Merck Sharp & Dohme LLC
Publication of JP2015501783A publication Critical patent/JP2015501783A/ja
Publication of JP2015501783A5 publication Critical patent/JP2015501783A5/ja
Application granted granted Critical
Publication of JP5857136B2 publication Critical patent/JP5857136B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
JP2014539998A 2011-11-03 2012-10-26 ｍＧｌｕＲ２−陰性アロステリック調節因子としてのキノリンカルボキサミドおよびキノリンカルボニトリル誘導体、組成物、およびその使用 Expired - Fee Related JP5857136B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161555227P 2011-11-03 2011-11-03
US61/555,227 2011-11-03
US201261672334P 2012-07-17 2012-07-17
US61/672,334 2012-07-17
PCT/US2012/062027 WO2013066736A1 (en) 2011-11-03 2012-10-26 QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2015242916A Division JP6114809B2 (ja) 2011-11-03 2015-12-14 ｍＧｌｕＲ２−陰性アロステリック調節因子としてのキノリンカルボキサミドおよびキノリンカルボニトリル誘導体、組成物、およびその使用

Publications (3)

Publication Number Publication Date
JP2015501783A JP2015501783A (ja) 2015-01-19
JP2015501783A5 JP2015501783A5 (enExample) 2015-12-24
JP5857136B2 true JP5857136B2 (ja) 2016-02-10

Family

ID=48192643

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2014539998A Expired - Fee Related JP5857136B2 (ja) 2011-11-03 2012-10-26 ｍＧｌｕＲ２−陰性アロステリック調節因子としてのキノリンカルボキサミドおよびキノリンカルボニトリル誘導体、組成物、およびその使用
JP2015242916A Expired - Fee Related JP6114809B2 (ja) 2011-11-03 2015-12-14 ｍＧｌｕＲ２−陰性アロステリック調節因子としてのキノリンカルボキサミドおよびキノリンカルボニトリル誘導体、組成物、およびその使用

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2015242916A Expired - Fee Related JP6114809B2 (ja) 2011-11-03 2015-12-14 ｍＧｌｕＲ２−陰性アロステリック調節因子としてのキノリンカルボキサミドおよびキノリンカルボニトリル誘導体、組成物、およびその使用

Country Status (16)

Country Link
US (3) US9278960B2 (enExample)
EP (1) EP2775841B1 (enExample)
JP (2) JP5857136B2 (enExample)
KR (1) KR20140088887A (enExample)
CN (1) CN104010504B (enExample)
AR (1) AR088611A1 (enExample)
AU (2) AU2012332895B2 (enExample)
CA (1) CA2853923A1 (enExample)
CO (1) CO6950474A2 (enExample)
IL (1) IL232291A0 (enExample)
IN (1) IN2014CN03234A (enExample)
MX (1) MX344308B (enExample)
MY (1) MY167423A (enExample)
RU (1) RU2610262C2 (enExample)
TW (1) TWI605040B (enExample)
WO (1) WO2013066736A1 (enExample)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9278960B2 (en) 2011-11-03 2016-03-08 Merck Sharp & Dohme Corp. Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators, compositions, and their use
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
JP6377245B2 (ja) * 2014-03-24 2018-08-22 グアンドン ジョンシェン ファーマシューティカル カンパニー リミテッド Ｓｍｏ阻害剤としてのキノリン誘導体
CN107001373B (zh) 2014-08-01 2020-01-07 詹森药业有限公司 6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮化合物及其作为MGLUR2受体的负向别构调节剂的用途
JO3601B1 (ar) 2014-08-01 2020-07-05 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
JOP20150177B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
JOP20150179B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
RU2708391C2 (ru) 2014-08-01 2019-12-06 Янссен Фармацевтика Нв 6,7-дигидропиразоло[1,5-а]пиразин-4(5h)-оновые соединения и их применение в качестве отрицательных аллостерических модуляторов рецепторов mglur2
WO2016029454A1 (en) * 2014-08-29 2016-03-03 Merck Sharp & Dohme Corp. TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
EP3000814A1 (en) 2014-09-26 2016-03-30 Domain Therapeutics Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors
AU2015357169B2 (en) 2014-12-03 2021-03-04 Janssen Pharmaceutica Nv Radiolabelled mGluR2 PET ligands
EP3227295B1 (en) 2014-12-03 2019-02-20 Janssen Pharmaceutica NV 6,7-dihydropyrazolo[1,5- ]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglu2 receptors
US10538491B2 (en) 2015-03-16 2020-01-21 Vanderbilt University 4,5-substituted picolinamide and picolinonitrile metabotropic glutamate receptor 2 negative allosteric modulators
CR20180109A (es) 2015-07-20 2018-05-03 Genzyme Corp Inhibidores de receptor del factor estimulador de colonias 1 (csf-1r)
CN108430986B (zh) 2015-10-26 2021-08-31 拜耳作物科学股份公司 作为有害生物控制剂的稠合双环杂环衍生物
RS60981B1 (sr) 2015-12-18 2020-11-30 Janssen Pharmaceutica Nv Radiooznačeni mglur2/3 pet ligandi
EA037941B1 (ru) 2015-12-18 2021-06-09 Янссен Фармацевтика Нв ЛИГАНДЫ mGluR2/3 ДЛЯ PET, МЕЧЕННЫЕ РАДИОАКТИВНЫМИ ИЗОТОПАМИ
SI3519416T1 (sl) * 2016-09-27 2021-08-31 Merck Sharp & Dohme Corp. Derivati kromana, izokromana in dihidroizobenzofurana kot mGluR2-negativni alosterični modulatorji, sestavki in njihova uporaba
MY201041A (en) 2017-11-24 2024-01-31 Sumitomo Pharma Co Ltd Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of group ii metabotropic glutamate receptor
CN108689957B (zh) * 2018-07-23 2020-07-03 南京药石科技股份有限公司 一种2r/2s-三氟甲基吗啉及其盐酸盐的制备方法和应用
EP3877356A4 (en) * 2018-11-09 2022-06-22 Vivace Therapeutics, Inc. BICYCLIC LINKS
AU2020257207B2 (en) 2019-04-16 2026-06-04 Vivace Therapeutics, Inc. Bicyclic compounds
EP3976027B1 (en) 2019-05-30 2025-11-05 Merck Sharp & Dohme LLC Quinoline derivatives as factor xi activation inhibitors
MX2021015872A (es) 2019-07-01 2022-02-03 UCB Biopharma SRL Un derivado de tetrahidroisoquinolina sustituido como modulador alosterico positivo de d1.
PH12021552825A1 (en) 2019-07-01 2022-10-03 UCB Biopharma SRL A substituted tetrahydroisoquinoline derivative as a d1 positive allosteric modulator
CN110256342B (zh) * 2019-07-16 2022-06-07 河南省科学院化学研究所有限公司 一种2-氰基喹啉衍生物的合成方法
ES3004257T3 (en) 2020-12-18 2025-03-12 UCB Biopharma SRL Prodrugs of 2-(3,5-dichloro-1-methyl-indazol-4-yl)-1-[(1s,3r)-3-(hydroxymethyl)-5-(1-hydroxy-1-methyl-ethyl)-1-methyl-3,4-dihydro-1h-isoquinolin-2-yl]ethanone
SI4263517T1 (sl) 2020-12-18 2025-01-31 UCB Biopharma SRL Substituiran tetrahidroizokinolinski derivat kot pozitivni alosterični modulator d1
US11530216B2 (en) 2020-12-23 2022-12-20 Genzyme Corporation Deuterated colony stimulating factor-1 receptor (CSF-1R) inhibitors
WO2024112853A1 (en) * 2022-11-24 2024-05-30 Exelixis, Inc. Compounds that inhibit pkmyt1
WO2025101691A1 (en) * 2023-11-08 2025-05-15 Exelixis, Inc. Methods for treating cancer using compounds that inhibit pkmyt1
CN119613413B (zh) * 2024-12-26 2026-02-06 上海皓元医药股份有限公司 一种非唑奈坦的制备方法

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0551831A1 (de) * 1992-01-15 1993-07-21 Hoechst Schering AgrEvo GmbH Verfahren zur Herstellung substituierter 2-Cyanopyridine
US5552437A (en) 1994-10-27 1996-09-03 Merck Frosst Canada, Inc. Bisarylcarbinol derivatives as inhibitors of leukotriene biosynthesis
US5576338A (en) * 1995-02-15 1996-11-19 Merck Frosst Canada, Inc. Bis (biaryl) compounds as inhibitors of leukotriene biosynthesis
GB9524137D0 (en) 1995-11-24 1996-01-24 Smithkline Beecham Spa Novel compounds
JPH115772A (ja) * 1997-04-25 1999-01-12 Takeda Chem Ind Ltd アミド誘導体、その製造法および用途
EP0975621A1 (en) * 1997-04-25 2000-02-02 Takeda Chemical Industries, Ltd. Cell differentiation inducing amide derivatives, their production and use
AU779874B2 (en) * 1999-10-15 2005-02-17 F. Hoffmann-La Roche Ag Benzodiazepine derivatives
TWI328009B (en) * 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
US20060275835A1 (en) 2003-07-11 2006-12-07 Jacobson Marlene A Methods for identifying cell surface receptor protein modulators
CN1856307A (zh) 2003-09-23 2006-11-01 默克公司 喹啉钾通道抑制剂
US20070287716A1 (en) 2004-10-28 2007-12-13 Hu Essa H Pyrimidine and Quinoline Potentiators of Metabotropic Glutamate Receptors
JP2009510132A (ja) * 2005-10-05 2009-03-12 メルク フロスト カナダ リミテツド ロイコトリエン生合成の阻害剤としての置換キノリン
AR065093A1 (es) 2007-02-05 2009-05-13 Merck Frosst Canada Ltd Compuestos farmacéuticos inhibidores de la biosintesis de leucotrienos
CN101730684B (zh) * 2007-06-18 2013-07-24 吉瑞工厂 磺酰基-喹啉衍生物
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
WO2012083866A1 (en) 2010-12-22 2012-06-28 The Hong Kong Polytechnic University Quinoline derivatives as anti-cancer agents
US9278960B2 (en) 2011-11-03 2016-03-08 Merck Sharp & Dohme Corp. Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators, compositions, and their use

Also Published As

Publication number Publication date
CA2853923A1 (en) 2013-05-10
US9636337B2 (en) 2017-05-02
US9278960B2 (en) 2016-03-08
RU2610262C2 (ru) 2017-02-08
EP2775841A1 (en) 2014-09-17
WO2013066736A1 (en) 2013-05-10
MX344308B (es) 2016-12-13
US20140309227A1 (en) 2014-10-16
AU2016200998B2 (en) 2017-04-06
AU2016200998A1 (en) 2016-03-03
JP6114809B2 (ja) 2017-04-12
US20160159744A1 (en) 2016-06-09
IN2014CN03234A (enExample) 2015-07-03
CN104010504A (zh) 2014-08-27
TW201321357A (zh) 2013-06-01
AR088611A1 (es) 2014-06-25
US20160158217A1 (en) 2016-06-09
CO6950474A2 (es) 2014-05-20
EP2775841A4 (en) 2015-05-06
NZ624596A (en) 2016-10-28
MX2014005415A (es) 2014-07-11
RU2014122335A (ru) 2015-12-10
EP2775841B1 (en) 2017-09-13
US9663506B2 (en) 2017-05-30
AU2012332895B2 (en) 2015-12-17
IL232291A0 (en) 2014-06-30
JP2015501783A (ja) 2015-01-19
TWI605040B (zh) 2017-11-11
CN104010504B (zh) 2016-04-06
AU2012332895A1 (en) 2014-05-15
KR20140088887A (ko) 2014-07-11
JP2016094447A (ja) 2016-05-26
MY167423A (en) 2018-08-27

Similar Documents

Publication Publication Date Title
JP6114809B2 (ja) ｍＧｌｕＲ２−陰性アロステリック調節因子としてのキノリンカルボキサミドおよびキノリンカルボニトリル誘導体、組成物、およびその使用
EP3185865B1 (en) Tetrahydronapthtyridine derivatives as mglur2 negative allosteric modulators, compositions, and their use.
TWI412525B (zh) 喹啉醯胺ｍ１受體之正向異位調節劑
CN102883723B (zh) 治疗化合物及相关的使用方法
JP6121658B2 (ja) 治療用化合物、及び関連する使用の方法
JP2012518640A (ja) ピラゾロ［４，３−ｃ］シンノリン−３−オンＭ１受容体陽性アロステリックモジュレーター
EP3684357B1 (en) Heteroaryl allosteric modulators of nicotinic acetylcholine receptors
EP3534889B1 (en) Substituted 6-membered aryl or heteroaryl allosteric modulators of nicotinic acetylcholine receptors
EP3534888B1 (en) Substituted bicyclic heteroaryl allosteric modulators of nicotinic acetylcholine receptors
US8653079B2 (en) Pyrazolo [4,3-C] cinnolin-3-one M1 receptor positive allosteric modulators
NZ624596B2 (en) QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
HK1181752A (en) Novel homopiperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20151013

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20151030

A871 Explanation of circumstances concerning accelerated examination

Free format text: JAPANESE INTERMEDIATE CODE: A871

Effective date: 20151030

TRDD Decision of grant or rejection written
A975 Report on accelerated examination

Free format text: JAPANESE INTERMEDIATE CODE: A971005

Effective date: 20151125

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20151208

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20151214

R150 Certificate of patent or registration of utility model

Ref document number: 5857136

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees